The present invention relates to a composition and method for treatment of patients afflicted with fibromyalgia. More particularly, this invention is directed to a composition and method for relieving symptoms associated with fibromyalgia in human patients by administering a combination of ubiquinone 10 and succinic acid.
Fibromyalgia is a common disabling disorder characterized by chronic musculoskeletal aches and pain, stiffness, and sleep abnormalities including diminished stage four sleep. Examination of affected patients reveals increased tenderness at muscle and tendon insertion sites, known as xe2x80x9ctender points.xe2x80x9d Fibromyalgia patients experience severe morning stiffness and a generalized decreased of overall physical function, and they arc often prone to headaches, memory and concentration problems, dizziness, numbness and tingling, and crampy abdominal or pelvic pain. Fibromyalgia affects 2-4% of the population and is most frequently found in women between 20 and 50 years old, although it can also affect men, the elderly and minors.
Diagnosis of fibromyalgia is often overlooked due to the general nature of the symptoms and the lack of diagnostic lab or x-ray abnormalities. The disorder is often concomitant with, masked by or confused with other diseases such as rheumatoid arthritis, chronic fatigue syndrome or irritable bowl syndrome. However, chronic fatigue syndrome (CFS) can be distinguished from fibromyalgia because patients with CFS are likely to have symptoms of viral illnesses such as fever, sore throat, and lymph node pain. A physician can positively diagnose fibromyalgia syndrome by finding the symptoms of musculoskeletal pain throughout the body and pain at more than 11 of 18 symmetrically distributed characteristic xe2x80x9ctender pointsxe2x80x9d when a finger pressure of about 4 kg is applied to the area, which test is known as the xe2x80x9ctender point index,xe2x80x9d or when tender points are detected with dolorimetry.
Currently the best treatment available for fibromyalgia consists of a combination of analgesics, sleep aids, exercise programs emphasizing stretching and cardiovascular fitness, relaxation techniques and other measures to reduce muscle tension, and educational programs to reduce emotional and physical stress. Numerous pharmaceutical regimens have been tried including treatment with serotonin modulators and antisera to endogenous psychoactive agents. Therapeutic response can be assessed by the reduction of pain in the tender point index and improvement in several generalized criteria such as physical function, stiffness, fatigue, depression, tenseness, etc. Responses to these various therapies have proven variable within a patient pool and have rarely exceeded modest relief of some symptoms. Often, initial therapeutic gains are temporary with the long term outcome marginally if at all distinguishable from placebo results.
Ubiquinone 10 and succinic acid are physiological substances present in all living cells. Succinic acid is oxidized to fumarate as one of the nine steps in the citric acid cycle, and oxidation of succinic acid results in the release of two electrons which are transferred to flavin adenine dinucleotide (FAD) to generate the reduced form of the molecule, FADH2. Electrons are then sequentially transferred between various flavin-linked dehydrogenases in the electron transport pathway localized on the inner mitochondrial membrane. Electron transport results in proton transport across the mitochondrial membrane and powers ATP synthesis through coupling with the oxidative phosphorylation pathway.
Ubiquinone 10 (CoQ10) is a lipophilic electron carrier that transports electrons between the various flavin-linked dehydrogenases in the electron transport pathway through reduction and oxidation of CoQ10. CoQ10 contains ten isoprene units in the multiprenyl side chain of the molecule which renders CoQ10 lipophilic and facilitates interaction of the molecule with the inner mitochondrial membrane where the components of the electron transfer chain are located. CoQ10 complexes with succinic acid and succinate dehydrogenase, the enzyme responsible for catalyzing the oxidation of succinic acid to fumarate, and acts as an electron carrier to facilitate the transfer of electrons from succinic acid to FAD. CoQ10 is widely distributed in tissues and may also act an antioxidant for such endogenous molecules as low density lipoproteins.
There exists a significant need for more effective therapy for patients afflicted with fibromyalgia. The present invention is directed to a method for treating a human patient suffering from fibromyalgia to produce a therapeutic response in the patient. The method comprises the step of administering to the patient ubiquinone 10 and succinic acid each at a dose of about 5 to about 500 mg/70 kg patient. In one embodiment of the invention the ubiquinone 10 and the succinic acid are each administered at a dose of about 50 to about 400 mg/70 kg patient and are administered by oral ingestion, bucally, sublingually, or parenterally. In another embodiment of the invention the ubiquinone 10 and succinic acid are each administered at a dose of about 50 to about 200 mg/70 kg patient. The ubiquinone 10 and succinic acid may be administered in a solid, liquid, or saliva-soluble dosage form, such as a lozenge. The daily doses can be divided into multiple doses administered one or more times per day.
In another embodiment, the invention provides a pharmaceutical composition comprising therapeutically effective amounts of ubiquinone 10 and succinic acid as the active ingredients, and a pharmaceutically acceptable carrier therefor. The pharmaceutical composition can be in the form of a liquid solution, a capsule, a caplet, a tablet, a gel-seal, or a lozenge and can be adapted for oral or parenteral administration.